Receptor rationales

Junghans and Siebler reported a series of 24 patients with recent stroke or TIA due to LAA and detected ES on TCD who were treated acutely with intravenous tirofiban, a GP Ilb/IIIa receptor antagonist. Median ES rate at baseline was 38 signals per hour. ES were abolished by tirofiban in all patients, and returned following cessation of infusion. Although preliminary, these data support the rationale for trials of acute GP Ilb/IIIa receptor blockade in patients with recently symptomatic LAA awaiting CEA. 

Fig. 11.4. Model for cholinergic signalling in the intestinal mucosa, providing a possible rationale for AChE secretion by parasitic nematodes. ACh released from enteric cholinergic motor neurons stimulates chloride secretion, mucus secretion and Paneth cell exocytosis through muscarinic receptors. Secretory responses may be modulated by mast cell mediators, either directly or via the induction of neural reflex programmes. The role of muscarinic receptor-positive cells in the lamina propria of rats infected with N. brasiliensis is undetermined, as are potential mechanisms of trans-epithelial transport of the enzymes. Adapted from Cooke (1984).

Dougall, I.G., Young, A., Ince, F., and Jackson, D.M., Dual dopamine D2 receptor and / -adrenoceptor agonists for the treatment of chronic obstructive pulmonary disease the pre-clinical rationale, Resp. Med., 97, S3, 2003. 

Sawynok J. (1995). Pharmacological rationale for the clinical use of caffeine. Drugs. 49(1) 37-50. Sawynok J. (1998). Adenosine receptor activation and nociception. Eur J Pharmacol. 347(1) 1-11. Schlaepfer TE, Strain EC, Greenberg BD, Preston KL, Lancaster E, Bigelow GE, Barta PE, Pearlson GD. (1998). Site of opioid action in the human brain mu and kappa agonists subjective and cerebral blood flow effects. Am J Psychiatry. 155(4) 470-73. 

The rationale for this type of contrast agent is to use the endogenous metabolic pathway of lipid metabolism in the liver for the transport of iodinated substances. Chylomicron remnants are naturally occurring lipoproteins in the blood that are responsible for the transport of lipids into the liver. Three different mechanisms for this transport are discussed direct uptake by the low-density lipoprotein receptor transport to the low-density lipoprotein receptor-related protein (LRP) mediated by heparan sulfate proteoglycan (HSPG) or direct HSPG-LRP uptake and direct HSPG uptake. One of the prerequisites for particles to be transported by these mechanisms is a mean diameter of less than 100-300 run. 

The rationale underlying the use of cholinergic compounds is that these are agonists of the nicotinic cholinergic receptor and therefore compensate for the low levels of ACh. Cholinergic compounds have been suggested as... 

Rationale for the Use of Progesterone Receptor Antagonists in Cancer Treatment... 

Holsboer F (1999) The rationale for corticotropin-releasing hormone receptor (CRH-R) antagonists to treat depression and anxiety. J Psychiatr Res 33 181-214... 

Neuropeptide Y (NPY) is a highly conserved 36 amino acid peptide of the pancreatic polypeptide family that is widely distributed throughout the mammalian brain. Y1 and Y2 receptors represent the major subtypes expressed in brain areas known to be activated upon anxiogenic stimulation, thus providing the rationale for studying the involvement of NPY and its receptor subtypes in anxiety-related behaviour (Kask et al. 2002). Other receptor subtypes in... 

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